Batefenterol

Non Chimik:

"(R)-1-(3-((2-chloro-4-(((2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino) methyl)-5-methoxyphenyl)amino)-3-oxopropyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate Batefenterol Succinate"

Kòd SMILES:

O=C(OC1CCN(CCC(NC2=CC(OC))=C(CNC[C@H](O)C3=CC=C(O)C4=C3C=CC(N4)=O)C=C2Cl)= O)CC1)NC5=CC=CC=C5C6=CC=CC=C6

Kòd InChi:

InChI=1S/C40H42ClN5O7/c1-52-36-22-33(31(41)21-26(36)23-42-24-35(48)29-11-13-34(47)39-30( 29)12-14-37(49)45-39)43-38(50)17-20-46-18-15-27(16-19-46)53-40(51)44-32-10- 6-5-9-28(32)25-7-3-2-4-8-25/h2-14,21-22,27,35,42,47-48H,15-20,23-24H2, 1H3,(H,43,50)(H,44,51)(H,45,49)/t35-/m0/s1

InChi kle:

URWYQGVSPQJGGB-DHUJRADRSA-N

Mot:

Batefenterol, TD-5959, GSK961081, 743461-65-6, GSK-961081, GSK 961081, TD5959, TD 5959, 743461-65-6

Solibilite:Soluble nan DMSO

Depo:0 - 4 ° C pou kout tèm (jou a semèn), oswa -20 ° C pou tèm long (mwa)

Deskripsyon:

Batefenterol se yon antagonist muscarinic ak β2-adrenergic reseptè (β2-AR) agonist (Kis = 1.4, 1.3, ak 3.7 nM, pou hM2, hM3, ak hβ2-AR, respektivman nan yon tès obligatwa radyoligand). Batefenterol montre aktivite agonist hβ2-AR ki pisan (EC50 = 0.29 nM) ak 440- ak 320-pliye selektivite fonksyonèl sou hβ1- ak hβ3-ARs, respektivman.1 Batefenterol pwovoke detant misk lis (EC50 = 11 nM) nan izole kochon Gine tracheal tisi ak inibit repons bronchoconstrictor nan yon tès bronchoprotection kochon Gine (ED50 = 6.4 µg/mL). Fòmasyon ki gen batefenterol yo nan esè klinik pou trete maladi obstriktif poumon kwonik (COPD).

Sib: β2-adrenoceptor